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Antiproliferative activities of halogenated thieno[3,2-d]pyrimidines.

ABSTRACT: The in vitro evaluation of thieno[3,2-d]pyrimidines identified halogenated compounds 1 and 2 with antiproliferative activity against three different cancer cell lines. A structure activity relationship study indicated the necessity of the chlorine at the C4-position for biological activity. The two most active compounds 1 and 2 were found to induce apoptosis in the leukemia L1210 cell line. Additionally, the compounds were screened against a variety of other microbial targets and as a result, selective activity against several fungi was also observed. The synthesis and preliminary biological results are reported herein.

SUBMITTER: Temburnikar KW

PROVIDER: S-EPMC4565497 | biostudies-literature | 2014 Apr

REPOSITORIES: biostudies-literature

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Antiproliferative activities of halogenated thieno[3,2-d]pyrimidines.

Temburnikar Kartik W KW Zimmermann Sarah C SC Kim Nathaniel T NT Ross Christina R CR Gelbmann Christopher C Salomon Christine E CE Wilson Gerald M GM Balzarini Jan J Seley-Radtke Katherine L KL

Bioorganic & medicinal chemistry 20140303 7

The in vitro evaluation of thieno[3,2-d]pyrimidines identified halogenated compounds 1 and 2 with antiproliferative activity against three different cancer cell lines. A structure activity relationship study indicated the necessity of the chlorine at the C4-position for biological activity. The two most active compounds 1 and 2 were found to induce apoptosis in the leukemia L1210 cell line. Additionally, the compounds were screened against a variety of other microbial targets and as a result, se ...[more]

PMID: 24631358

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